Cargando…
Structure Kinetics Relationships and Molecular Dynamics Show Crucial Role for Heterocycle Leaving Group in Irreversible Diacylglycerol Lipase Inhibitors
[Image: see text] Drug discovery programs of covalent irreversible, mechanism-based enzyme inhibitors often focus on optimization of potency as determined by IC(50)-values in biochemical assays. These assays do not allow the characterization of the binding activity (K(i)) and reactivity (k(inact)) a...
| Autores principales: | , , , , , |
|---|---|
| Formato: | Online Artículo Texto |
| Lenguaje: | English |
| Publicado: |
American Chemical
Society
2019
|
| Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6745892/ https://www.ncbi.nlm.nih.gov/pubmed/31437392 http://dx.doi.org/10.1021/acs.jmedchem.9b00686 |